DBPR108 is a potent, selective, and orally bioavailable dipeptide-derived inhibitor of DPP4 with IC50 of 15 nM; no inhibition on DDP8 and DPP9.IC50 value: 15 nM [1]Target: DPP4 inhibitorDBPR108 is an IC50=15 nM DPP IV inhibitor displays a more than 3000-fold selectivity over DPP8 DPP9, FAP and DPP-II. TThe in vivo effects of DBPR108, including inhibition of plasma DPP-IV activity and suppression of blood glucose elevation, were also demonstrated. DBPR108 is a potent, selective, long-acting and safe DPP-IV inhibitor as a potential treatment of type 2 diabetesmellitus.
References:
[1]. Yeh TK, et al. (2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV. Bioorg Med Chem Lett. 2010 Jun